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The modulation of the activity of tyrosine kinases (TK) is an appealing topic of current research. This work presents new pseudopeptidic cages that protect the substrates from the action of the TK enzyme, precluding the corresponding Tyr phosphorylation, with a very good correlation between the Tyr caging and the kinase inhibition. The results illustrate how TK signaling can be efficiently and selectively...
The selective recognition of tyrosine residues in peptides is an appealing approach to inhibiting their tyrosine kinase (TK)‐mediated phosphorylation. Herein, we describe pseudopeptidic cages that efficiently protect substrates from the action of the Src TK enzyme, precluding the corresponding Tyr phosphorylation. Fluorescence emission titrations show that the most efficient cage inhibitors strongly...